1,3dibromo5,5dimethylhydantoin

1,3-Dibromo-5,5-dimethylhydantoin is an alkyl chain-based PROTAC linker utilized in PROTAC synthesis.

Thalidomide 5-fluoride (H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-5-fluoro-) is a thalidomide-based Cereblon ligand that binds to the IRAK4 protein ligand via a linker to form PROTACIRAK4 degrader-1.

Bis-propargyl-PEG6 is a polyethylene glycol (PEG) derivative commonly employed as a PEG-based PROTAC linker during the synthesis of PROTACs. Its application includes the generation of polymer-linked multimers of guanosine-3', 5'-cyclic monophosphates[1].

Bis-propargyl-PEG7 is a polyethylene glycol (PEG)-based linker utilized in the synthesis of proteolysis targeting chimeras (PROTACs). It is particularly employed for the synthesis of polymer-linked multimers of guanosine-3',5'-cyclic monophosphates[1].

Propargyl-PEG5-acid is a non-cleavable 5-unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs) and can be employed to create ADC inhibitors of Galectin-3 [1].

(S,R,S)-AHPC-PEG3-NH2 is a synthetic conjugate composed of the (S,R,S)-AHPC VHL ligand and a 3-unit PEG linker, utilized in PROTAC technology as an E3 ligase ligand-linker.

YB-3-17 is a bifunctional molecule that can inhibit mTOR with an IC50 of 0.22 nM or degrade the G1 to S phase transition 1 gene (GSPT1) through the PROTAC mechanism, with a DC50 of 5 nM. It exhibits antiproliferative activity at nanomolar concentrations in various glioblastoma cell lines. Additionally, YB-3-17 shows antitumor activity in mouse models. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase Cereblon)

PROTAC ER Degrader-14 (compound 86) is a PROTAC-type estrogen receptor ERR degrader. It comprises an E3 ubiquitin ligase ligand (blue part) (S)-Deoxy-thalidomide, a PROTAC linker (black part) N-Boc-piperazine, and a target protein ligand (red part) ER ligand-6. The combination of the E3 ligase and linker forms tert-Butyl (S)-4-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperazine-1-carboxylate.

KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM for IRAK4 and 5 nM for Ikaros. It effectively induces apoptosis in MYD88 MT DLBCL and has demonstrated efficacy in inducing in vivo tumor regressions in a lymphoma model [1] [2] [3].

PROTAC α-synuclein degrader 3 (compound 5) is a potent and selective agent for degrading α-synuclein, used in Parkinson's disease research [1].

PROTAC SMARCA2 4-degrader-26 is a PROTAC targeting the SMARCA2 4 proteins. It is composed of the ligand for PROTAC targeting proteins, 2-(4-(3-Amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetic acid, an E3 ligase component (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, and a PROTAC linker (S)-2-Amino-3,3-dimethylbutanoic acid. The coupled complex of the E3 ubiquitin ligase ligand + Linker is referred to as (S,R,S)-AHPC.